Pharmacokinetics, tissue distribution and excretion study of resveratrol and its prodrug 3,5,4′-tri-O-acetylresveratrol in rats

Li, Liang; Liu, Xueying; Wang, Qingwei; Cheng, Sikun; Zhang, Shengyong; Zhang, Meng

doi:10.1016/j.phymed.2012.12.012

Cited by 86 publications

(70 citation statements)

References 14 publications

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“…Future investigations may address issues of optimization of oral bioavailability by considering alternative formulations (Amri et al, 2012), the use of resveratrol derivatives with higher oral availability, such as pterostilbene (e.g. Yeo et al, 2013), and since only relatively little resveratrol appears to find its way to the brain (Liang et al, 2013;Sale et al, 2004), the role of the parent compound relative to its metabolites, also known to be active (cf. Amri et al, 2012 In addition to the pharmacological normalization of the peripubertal stress-induced social deficit, the present study identified alterations in certain prefrontal cortex subregions following resveratrol treatment.…”

Section: Discussionmentioning

confidence: 99%

Social deficits induced by peripubertal stress in rats are reversed by resveratrol

Poirier

Imamura

Zanoletti

et al. 2014

Journal of Psychiatric Research

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a b s t r a c tAdolescence is increasingly recognized as a critical period for the development of the social system, through the maturation of social competences and of their underlying neural circuitries. The present study sought to test the utility of resveratrol, a dietary phenol recently reported to have mood lifting properties, in modulating social interaction that is deficient following early life adversity. The main aims were to 1) pharmacologically restore normative social investigation levels dampened by peripubertal stress in rats and 2) identify neural pathways engaged by this pharmacological approach. Following peripubertal (P28e42) stress consisting of unpredictable exposures to fearful experiences, at adulthood the subjects' propensity for social exploration was examined in the three-chamber apparatus, comparing time invested in social or non-social investigation. Administered intraperitoneally 30 min before testing, resveratrol (20 mg/kg) normalized the peripubertal stress-induced social investigation deficit seen in the vehicle group, selectively altering juvenile but not object exploration. Examination of prefrontal cortex subregion protein samples following acute resveratrol treatment in a separate cohort revealed that while monoamine oxidase A (MAOA) enzymatic activity remained unaltered, nuclear AKT activation was selectively increased in the infralimbic cortex, but not in the prelimbic or anterior cingulate cortex. In contrast, androgen receptor nuclear localization was increased in the prelimbic cortex, but not in the infralimbic or anterior cingulate cortex. This demonstration that social contact deficits are reversed by resveratrol administration emphasizes a prosocial role for this dietary phenol, and evokes the possibility of developing new treatments for social dysfunctions.

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Section: Discussionmentioning

confidence: 99%

Social deficits induced by peripubertal stress in rats are reversed by resveratrol

Poirier

Imamura

Zanoletti

et al. 2014

Journal of Psychiatric Research

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“…It has been documented that the high rate of the first-pass metabolism of drug, variable rate of gastric emptying and motility of the gastrointestinal tract may result in low bioavailability of the drug. The variation in degrees of drug response to the absorption site also influences the bioavailability (Liang et al 2013). For the oral route of administration, metabolism in the intestinal membrane and the liver is of major concern as it can reduce the systemic bioavailability of the drug (Kushwaha et al 2014).…”

Section: Discussionmentioning

confidence: 99%

“…It has been reported that approximately 30-40% of the new drug candidates failed during drug development process due to their poor pharmacokinetic properties (Grimaldi et al 1990;Liang et al 2013). Thus, animal models play a crucial role in understanding the pharmacokinetic properties of novel drugs (Kandhare et al 2011).…”

Section: Introductionmentioning

confidence: 99%

Development and validation of HPLC method for vicenin-1 isolated from fenugreek seeds in rat plasma: application to pharmacokinetic, tissue distribution and excretion studies

Kandhare

Bodhankar

Thakurdesai

2016

Pharmaceutical Biology

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Context: Vicenin-1, a flavonol glycoside, has potent platelet aggregation inhibition, antioxidant, radioprotectants and anti-inflammatory activities. Objective: To establish a rapid, simple, precise and sensitive high-performance liquid chromatography (HPLC) method for determination of vicenin-1 in rat plasma, and to investigate the pharmacokinetics, tissue distribution and excretion after a single 60 mg/kg oral dose in rats. Materials and methods: Vicenin-1 was extracted by solid-liquid extraction through Tulsicon V R ADS-400 (0.40-1.2 mm). Chromatographic separation was achieved by HPLC with a C 18 column with a mobile phase composed of water and acetonitrile (75:25 v/v) and a flow rate of 1 mL/min along with UV detection at 210 nm. Results: Good linearity of calibration curve was found between 10.5 and 100.5 lg/mL (R 2 ¼ 0.995) for plasma and tissue, whereas 2.5-500 lg/mL (R 2 ¼ 0.999) for the urine and stool samples. The extraction recoveries were 98.51-99.58% for vicenin-1 in plasma, whereas intra-day and inter-day precision were validated by relative standard deviation (%RSD), that came in the ranges of 1.16-1.79% and 1.28-1.73%, respectively. The pharmacokinetics results showed C max (7.039 lg/mL) and T max (2 h) after oral administration of vicenin-1. Tissue distribution study showed that the highest concentration of vicenin-1 was achieved in the liver followed by the lung. Approximately 24.2% of its administered dose was excreted via urinary excretion route. Conclusion: The first-pass metabolism, poor solubility and presence of reducing sugar moiety in vicenin-1 may decrease its bioavailability. The developed method is sensitive, specific and was successfully applied to the pharmacokinetics, tissue distribution and excretion studies of vicenin-1 in rats.ARTICLE HISTORY

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“…Subsequent clinical trials are currently investigating this dose limit [307,310]. Resveratrol's poor bioavailability is a significant issue with regard to extrapolating its effects to humans, and various approaches have been created to enhance its bioavailability [311], including consuming it with various foods [312], using it in combination with an additional phytochemical piperine [313], and using a prodrug approach [314], micronized powders [315,316], or nanotechnological formulations [317][318][319].…”

Section: Clinical Trials With Resveratrolmentioning

confidence: 99%

Chemically-Induced DNA Damage, Mutagenesis, and Cancer

2018

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Pharmacokinetics, tissue distribution and excretion study of resveratrol and its prodrug 3,5,4′-tri-O-acetylresveratrol in rats

Cited by 86 publications

References 14 publications

Social deficits induced by peripubertal stress in rats are reversed by resveratrol

Social deficits induced by peripubertal stress in rats are reversed by resveratrol

Development and validation of HPLC method for vicenin-1 isolated from fenugreek seeds in rat plasma: application to pharmacokinetic, tissue distribution and excretion studies

Chemically-Induced DNA Damage, Mutagenesis, and Cancer

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